Target Validation Information
Target ID T31204
Target Name 5-hydroxytryptamine 2B receptor
Target Type
Successful
Drug Potency against Target ADS-103274 Drug Info IC50 = 1500 nM [528581]
7,8,9,10-tetrahydro-6H-furo-[2,3-g][3]benzazepine Drug Info Ki = 34 nM [529221]
WAY-181187 Drug Info Ki = 458 nM [529112]
1-((R)-2-aminopropyl)-1H-indazol-6-ol Drug Info Ki = 35 nM [527952]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [531079]
Minaprine Drug Info Ki = 17000 nM [536549]
CHLOROPHENYLPIPERAZINE Drug Info Ki = 24 nM [530589]
VER-5593 Drug Info Ki = 21 nM [527037]
VER-5384 Drug Info Ki = 49 nM [527037]
(2S)-1-(6-methoxy-1H-indazol-1-yl)propan-2-amine Drug Info Ki = 7.5 nM [527952]
3-(2-Dimethylamino-ethyl)-1-methyl-1H-indol-4-ol Drug Info Ki = 38 nM [527668]
3-Dimethylaminomethyl-1H-indol-4-ol Drug Info Ki = 1242 nM [527668]
1-((S)-2-aminopropyl)-1H-indazol-6-ol Drug Info Ki = 8.1 nM [527952]
3-(2-Amino-propyl)-1H-indol-5-ol Drug Info Ki = 13 nM [527952]
5-MEO-DMT Drug Info Ki = 52 nM [527952]
[2-(4-Fluoro-1H-indol-3-yl)-ethyl]-dimethyl-amine Drug Info Ki = 8.39 nM [527668]
1-Butyl-3-(2-dimethylamino-ethyl)-1H-indol-4-ol Drug Info Ki = 5.8 nM [527668]
SEROTONIN Drug Info Ki = 12 nM [527833]
ADRENOGLOMERULOTROPIN Drug Info Ki = 491 nM [531223]
BP-897 Drug Info Ki = 33.1 nM [531223]
(+/-)-nantenine Drug Info Ki = 543 nM [530558]
VER-2692 Drug Info Ki = 12 nM [527833]
(5-methoxy-1H-indol-3-yl)methanamine Drug Info Ki = 1617 nM [531223]
1-((S)-2-aminopropyl)-7-fluoro-1H-indazol-6-ol Drug Info Ki = 1.7 nM [527952]
YM-348 Drug Info Ki = 2.5 nM [529221]
7,8,9,10-tetrahydro-6H-furo-[3,2-g][3]benzazepine Drug Info Ki = 90 nM [529221]
2-(5-Methoxy-1H-indol-3-yl)-1-methyl-ethylamine Drug Info Ki = 7.8 nM [527952]
Racemic DOI Drug Info IC50 = 3.5 nM [529789]
3-(2-Pyrrolidin-1-yl-ethyl)-1H-indol-4-ol Drug Info Ki = 423 nM [527668]
1-((S)-2-aminopropyl)-7-iodo-1H-indazol-6-ol Drug Info Ki = 6 nM [527952]
1-((S)-2-aminopropyl)-7-methyl-1H-indazol-6-ol Drug Info Ki = 8.7 nM [527952]
3-(2-Dimethylamino-propyl)-1H-indol-4-ol Drug Info Ki = 745 nM [527668]
1-((S)-2-aminopropyl)-7-chloro-1H-indazol-6-ol Drug Info Ki = 3.8 nM [527952]
3-(2-Dimethylamino-ethyl)-1H-indol-6-ol Drug Info Ki = 6300 nM [527668]
ADS-103253 Drug Info IC50 = 1900 nM [528581]
AR-129330 Drug Info IC50 = 9.66 nM [530396]
VER-3323 Drug Info Ki = 46 nM [527037]
Ro-60-0175 Drug Info Ki = 5.1 nM [527833]
FENDILINE Drug Info Ki = 3217 nM [531223]
6-Fluoromelatonin Drug Info Ki = 2495 nM [531223]
1-(2-aminoethyl)-1H-indazol-6-ol Drug Info Ki = 15 nM [527952]
3-Dimethylaminomethyl-1-methyl-1H-indol-4-ol Drug Info Ki = 1242 nM [527668]
3-(3-Dimethylamino-propyl)-1H-indol-4-ol Drug Info Ki = 98 nM [527668]
6,7-dichloro-2,3,4,5-tetrahydro-1H-3-benzazepine Drug Info Ki = 100 nM [529221]
Action against Disease Model Triflupromazine IC50 on pancreatic beta-cell ATP-sensitive potassi uM channels: 4000nM [552614] Drug Info
References
Ref 528581Bioorg Med Chem Lett. 2007 Mar 1;17(5):1403-7. Epub 2006 Dec 2.Quinazoline and benzimidazole MCH-1R antagonists.
Ref 529221Bioorg Med Chem. 2008 Mar 15;16(6):3309-20. Epub 2007 Dec 8.Synthesis and structure-activity relationships of a series of benzazepine derivatives as 5-HT2C receptor agonists.
Ref 529112J Med Chem. 2007 Nov 15;50(23):5535-8. Epub 2007 Oct 19.Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT(6) receptor agonist.
Ref 527952J Med Chem. 2006 Jan 12;49(1):318-28.1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.
Ref 531079J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
Ref 536549Privileged structures: a useful concept for the rational design of new lead drug candidates. Mini Rev Med Chem. 2007 Nov;7(11):1108-19.
Ref 530589Bioorg Med Chem Lett. 2010 Feb 1;20(3):1128-33. Epub 2009 Dec 6.Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents.
Ref 527037Bioorg Med Chem Lett. 2004 May 3;14(9):2367-70.Indoline derivatives as 5-HT(2C) receptor agonists.
Ref 527037Bioorg Med Chem Lett. 2004 May 3;14(9):2367-70.Indoline derivatives as 5-HT(2C) receptor agonists.
Ref 527952J Med Chem. 2006 Jan 12;49(1):318-28.1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.
Ref 527668Bioorg Med Chem Lett. 2005 Oct 15;15(20):4555-9.SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist.
Ref 527668Bioorg Med Chem Lett. 2005 Oct 15;15(20):4555-9.SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist.
Ref 527952J Med Chem. 2006 Jan 12;49(1):318-28.1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.
Ref 527952J Med Chem. 2006 Jan 12;49(1):318-28.1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.
Ref 527952J Med Chem. 2006 Jan 12;49(1):318-28.1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.
Ref 527668Bioorg Med Chem Lett. 2005 Oct 15;15(20):4555-9.SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist.
Ref 527668Bioorg Med Chem Lett. 2005 Oct 15;15(20):4555-9.SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist.
Ref 527833Bioorg Med Chem Lett. 2006 Feb;16(3):677-80. Epub 2005 Oct 27.Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists.
Ref 531223J Med Chem. 2010 Nov 11;53(21):7573-86.Development, validation, and use of quantitative structure-activity relationship models of 5-hydroxytryptamine (2B) receptor ligands to identify novel receptor binders and putative valvulopathic compounds among common drugs.
Ref 531223J Med Chem. 2010 Nov 11;53(21):7573-86.Development, validation, and use of quantitative structure-activity relationship models of 5-hydroxytryptamine (2B) receptor ligands to identify novel receptor binders and putative valvulopathic compounds among common drugs.
Ref 552614Chlorpromazine and related phenothiazines inhibit the ATP-sensitive K+ channel. Eur J Pharmacol. 1991 May 30;198(1):101-4.
Ref 530558Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. Epub 2009 Nov 20.Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.
Ref 527833Bioorg Med Chem Lett. 2006 Feb;16(3):677-80. Epub 2005 Oct 27.Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists.
Ref 531223J Med Chem. 2010 Nov 11;53(21):7573-86.Development, validation, and use of quantitative structure-activity relationship models of 5-hydroxytryptamine (2B) receptor ligands to identify novel receptor binders and putative valvulopathic compounds among common drugs.
Ref 527952J Med Chem. 2006 Jan 12;49(1):318-28.1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.
Ref 529221Bioorg Med Chem. 2008 Mar 15;16(6):3309-20. Epub 2007 Dec 8.Synthesis and structure-activity relationships of a series of benzazepine derivatives as 5-HT2C receptor agonists.
Ref 529221Bioorg Med Chem. 2008 Mar 15;16(6):3309-20. Epub 2007 Dec 8.Synthesis and structure-activity relationships of a series of benzazepine derivatives as 5-HT2C receptor agonists.
Ref 527952J Med Chem. 2006 Jan 12;49(1):318-28.1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.
Ref 529789J Med Chem. 2008 Nov 27;51(22):7094-8.cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.
Ref 527668Bioorg Med Chem Lett. 2005 Oct 15;15(20):4555-9.SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist.
Ref 527952J Med Chem. 2006 Jan 12;49(1):318-28.1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.
Ref 527952J Med Chem. 2006 Jan 12;49(1):318-28.1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.
Ref 527668Bioorg Med Chem Lett. 2005 Oct 15;15(20):4555-9.SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist.
Ref 527952J Med Chem. 2006 Jan 12;49(1):318-28.1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.
Ref 527668Bioorg Med Chem Lett. 2005 Oct 15;15(20):4555-9.SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist.
Ref 528581Bioorg Med Chem Lett. 2007 Mar 1;17(5):1403-7. Epub 2006 Dec 2.Quinazoline and benzimidazole MCH-1R antagonists.
Ref 530396Bioorg Med Chem Lett. 2009 Nov 1;19(21):6166-71. Epub 2009 Sep 6.Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation.
Ref 527037Bioorg Med Chem Lett. 2004 May 3;14(9):2367-70.Indoline derivatives as 5-HT(2C) receptor agonists.
Ref 527833Bioorg Med Chem Lett. 2006 Feb;16(3):677-80. Epub 2005 Oct 27.Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists.
Ref 531223J Med Chem. 2010 Nov 11;53(21):7573-86.Development, validation, and use of quantitative structure-activity relationship models of 5-hydroxytryptamine (2B) receptor ligands to identify novel receptor binders and putative valvulopathic compounds among common drugs.
Ref 531223J Med Chem. 2010 Nov 11;53(21):7573-86.Development, validation, and use of quantitative structure-activity relationship models of 5-hydroxytryptamine (2B) receptor ligands to identify novel receptor binders and putative valvulopathic compounds among common drugs.
Ref 527952J Med Chem. 2006 Jan 12;49(1):318-28.1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.
Ref 527668Bioorg Med Chem Lett. 2005 Oct 15;15(20):4555-9.SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist.
Ref 527668Bioorg Med Chem Lett. 2005 Oct 15;15(20):4555-9.SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist.
Ref 529221Bioorg Med Chem. 2008 Mar 15;16(6):3309-20. Epub 2007 Dec 8.Synthesis and structure-activity relationships of a series of benzazepine derivatives as 5-HT2C receptor agonists.

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